Table 2.
NVP-CGM097 sensitized ABCB1-gene-transfected cells to ABCB1 substrates.
| Treatment | IC50 ± SDa (RFb)(μM) | |
|---|---|---|
| HEK293/pcDNA3.1 | HEK293/ABCB1 | |
| Doxorubicin | 0.012 ± 0.004 (1.00) | 0.289 ± 0.081 (24.08) |
| +NVP CGM097 (1 μM) | 0.014 ± 0.004 (1.17) | 0.123 ± 0.017 (10.25)* |
| +NVP CGM097 (3 μM) | 0.017 ± 0.014 (1.42) | 0.043 ± 0.004 (3.58)* |
| +Verapamil (3 μM) | 0.015 ± 0.003 (1.25) | 0.066 ± 0.002 (5.50)* |
| Paclitaxel | 0.016 ± 0.004 (1.00) | 0.865 ± 0.260 (54.06) |
| +NVP CGM097 (1 μM) | 0.020 ± 0.009 (1.25) | 0.211 ± 0.028 (13.19)* |
| +NVP CGM097 (3 μM) | 0.014 ± 0.004 (0.88) | 0.025 ± 0.002 (1.56)* |
| +Verapamil (3 μM) | 0.019 ± 0.001 (1.19) | 0.030 ± 0.002 (1.88)* |
| Cisplatin | 1.228 ± 0.093 (1.00) | 1.184 ± 0.133 (0.96) |
| +NVP CGM097 (1 μM) | 1.364 ± 0.098 (1.11) | 1.213 ± 0.067 (0.99) |
| +NVP CGM097 (3 μM) | 1.104 ± 0.164 (0.90) | 1.025 ± 0.039 (0.83) |
| +Verapamil (3 μM) | 1.705 ± 0.187 (1.39) | 0.972 ± 0.131 (0.80) |
a
IC50 values were determined by MTT assay as described in “Materials and Methods,” and were obtained from three independent experiments in triplicate.
b
Resistance fold (RF) was calculated from dividing the IC50 values of resistant cells (HEK293/ABCB1) by the IC50 of parental cells (HEK293/pcDNA3.1) in the presence or absence of NVP-CGM097 or positive control inhibitor.
*
p < 0.05 vs. group treated with antineoplastic drug only.